The present invention relates to 1,4-dihydropyridine derivatives having superior vasodilative and platelet aggregation inhibiting activities.
Some of 1,4-dihydropyridine-3,5-dicarboxylate compounds have vasodilative effects based on the calcium entry blocking action and therefore are employed as coronary vasodilators, ameliorants of cerebral circulation, and hypotensive drugs.
Representative examples of such compounds are 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)pyridine-3,5-dicarboxylic acid dimethyl ester (generally referred to as "NIFEDIPINE"; U.S. Pat. No. 3,644,627) and 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid-3-[2-(N-benzyl-N-methylamino)ethyl]ester-5-methyl ester hydrochloride (generally referred to as "NICARDIPINE"; Japanese Patent Publication 55-45075).
In addition, 1,4-dihydropyridine compounds having both vasodilative based on the calcium entry blocking action and platelet aggregation inhibitory activities, are now being developed as disclosed, for example, in Japanese Laid-Open Patent Applications Nos. 56-140989, 60-215684, 61-10576, 61-5076, 61-197578, 60-226876, 61-47477, 61-212581, and 62-187468.
1,4-dihydropyridine compounds such as NIFEDIPINE and NICARDIPINE have high vasolidative activity based on the calcium entry blocking action, but are not satisfactory as remedy for atherosclerosis. Therefore, researches are being made for obtaining 1,4-dihydropyridine derivatives having not only vasodilating activity, but also platelet aggregation inhibitory activity, capable of inhibiting platelet aggregation and preventing and curing atherosclerosis, which can be used as remedies for circulatory system. However, satisfactory remedies having the above-mentioned activities have not been found yet.